Adverse Drug Reaction Classification System

         

Pharmaceutical Information
Drug Name Osimertinib
Drug ID BADD_D01629
Description Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals. Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in cases where tumour EGFR expression is positive for the T790M mutation as detected by FDA-approved testing and which has progressed following therapy with a first-generation EGFR tyrosine kinase inhibitor. Approximately 10% of patients with NSCLC have a rapid and clinically effective response to EGFR-TKIs due to the presence of specific activating EGFR mutations within the tumour cells. More specifically, deletions around the LREA motif in exon 19 and exon 21 L858R point mutations are correlated with response to therapy. Development of third-generation EGFR-TKIs, such as osimertinib, has been in response to altered tumour resistance patterns following treatment and toxic side effects that impact patient quality of life. Treatment with first-generation EGFR-TKIs (gefitinib and erlotinib) has been associated with the development of resistance through activating mutations in the EGFR gene. Second-generation EGFR-TKIs (afatinib and dacomitinib) were then developed to be more potent inhibitors, although their use is associated with increased toxicity through nonspecific targeting of wild-type EGFR. In contrast, third-generation inhibitors are specific for the gate-keeper T790M mutations which increases ATP binding activity to EGFR and result in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity.
Indications and Usage Osimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy.
Marketing Status approved
ATC Code L01EB04
DrugBank ID DB09330
KEGG ID D10766
MeSH ID C000596361
PubChem ID 71496458
TTD Drug ID D0O8GK
NDC Product Code 0310-1353; 0310-1350; 0310-1354; 54864-844; 17228-1349; 17228-1350; 0310-1349
UNII 3C06JJ0Z2O
Synonyms osimertinib | Tagrisso | AZD9291
Chemical Information
Molecular Formula C28H33N7O2
CAS Registry Number 1421373-65-0
SMILES CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice.
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Metastasis16.22.01.0010.000951%-
Renal impairment20.01.03.0100.001981%-
Malignant transformation16.16.01.0130.001511%-
Bone marrow failure01.03.03.0050.001007%
Cytopenia01.03.03.0120.000358%-
Liver injury09.01.07.022; 12.01.17.0120.000504%-
Organising pneumonia22.01.02.0080.000168%-
Tumour compression16.32.03.0210.000112%-
Oropharyngeal pain07.05.05.004; 22.12.03.016--
Drug-induced liver injury09.01.07.023; 12.03.01.0440.001119%-
Cornea verticillata06.06.03.0160.000381%-
Cholangitis acute09.02.01.0060.000112%-
Chronic gastritis07.08.02.005; 10.04.04.011; 11.07.01.0160.000168%-
Drowning08.04.01.014; 12.01.18.0030.000112%-
Lung carcinoma cell type unspecified stage IV16.19.02.006; 22.08.01.0190.000112%-
Lymphadenopathy mediastinal01.09.01.025; 22.09.03.0060.000224%-
Malignant ascites07.07.01.004; 16.32.03.0130.000112%-
Malignant pleural effusion16.32.03.014; 22.05.04.0010.000504%-
Metastases to adrenals05.01.04.007; 16.22.02.0120.000448%-
Metastases to bone15.09.03.006; 16.22.02.0050.002295%-
Metastases to kidney16.22.02.017; 20.01.04.0100.000112%-
Metastases to lymph nodes01.09.01.015; 16.22.02.0060.000672%-
Metastases to pleura16.22.02.022; 22.05.04.0020.000224%-
Metastases to the mediastinum16.22.02.027; 22.09.03.0090.000112%-
Pulmonary artery thrombosis22.06.02.005; 24.01.06.0050.000168%-
Pericardial effusion malignant02.06.01.009; 16.32.03.0260.000168%-
Mechanical ileus07.13.01.0140.000112%-
Metastases to thorax16.22.02.028; 22.08.03.0010.000112%-
Metastases to meninges16.22.02.003; 17.02.10.0120.003470%-
Lymphangiosis carcinomatosa01.09.01.027; 16.22.02.009; 24.09.02.0070.000839%-
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